Pfizer Inc.

在当今科技飞速发展的时代，人工智能（AI）正以前所未有的速度渗透到各个领域，制药行业也不例外。AI 技术的应用为制药领域带来了诸多变革，从药物研发到个性化医疗，再到制药生产的各个环节，都产生了深远影响。 AI 在制药行业的发展历程 AI 在制药行业的应用经历了从基础到前沿的发展历程。早在 20 世纪 80 - 90 年代，AI 在药物研发中的应用还局限于基础计算模型，主要用于分子建模和化学结构预测。到了 21 世纪初，机器学习算法的引入助力药物研发，能够分析复杂数据集，预测分子相互作用和优化药物配方。2010 年代，随着大数据、深度学习技术的发展以及大量生物和化学数据集的涌现，AI 在制药行业得到了广泛应用，加速药物研发进程。 AI 在药物研发中的应用 靶点识别与验证 药物研发的首要步骤是识别疾病靶点，AI 技术在此发挥了关键作用。通过分析大量基因组、蛋白质组和临床数据，AI 算法能够精准找出潜在的疾病相关靶点，并对其进行优先级排序。例如，阿斯利康的基因组研究中心借助 AI 算法，对大量基因组序列进行分析，以识别可能导致疾病的基因变异、基因、信号通路等，为开发更有效的药物奠定基础，这一技术在 CRISPR 基因编辑技术中也发挥了重要作用。药物分子设计与优化 AI 算法能够预测潜在药物候选分子的结构和性质，设计出与靶点相互作用的分子。深度思维（DeepMind）的 AlphaFold 算法利用深度学习，在预测蛋白质结构方面展现出了极高的准确性，为理解蛋白质 - 配体相互作用提供了有价值的信息。同时，AI 还能通过生成对抗网络（GANs）等技术，全新设计具有更高效力和选择性的药物分子，加速药物研发进程。虚拟筛选 虚拟筛选是药物研发早期的关键环节，传统方法存在局限性。机器学习算法为虚拟筛选提供了更强大、灵活的方法，能够分析各种化学特征，更精确地预测配体 - 靶点结合。通过对大量化学化合物和生物靶点数据的学习，机器学习模型可以识别出与结合亲和力相关的微妙结构特征和物理化学性质，提高虚拟筛选的准确性和效率。AI 在个性化医疗中的应用预测药物反应与优化治疗方案 利用机器学习和深度学习算法，结合患者的基因组、蛋白质组和代谢组等生物数据，能够预测不同患者对特定药物的反应。通过持续学习患者的治疗反应，AI 算法可以实时调整药物剂量和治疗方案，提高治疗效果。不过，AI 模型在生物学机制解释方面存在不足，一些研究正在努力解决这一问题，如开发可解释的深度学习模型 DrugCell。基于个体特征的精准治疗 AI 在个性化医疗中的另一个重要应用是根据患者的遗传背景、生活方式和其他因素制定个性化治疗方案。在药物基因组学领域，AI 算法可以根据患者的基因组成预测其对不同药物的反应，指导药物选择和剂量调整。此外，AI 还能综合考虑生活方式因素、社会经济状况等，提供更全面的个性化医疗服务。 AI 在药物制剂与递送中的应用优化药物制剂与辅料选择 AI 预测模型可优化药物制剂，确保活性成分高效送达靶点。通过分析大量数据，AI 能预测药物从特定制剂中的释放曲线，设计出能提供稳定治疗效果的控释制剂。在辅料选择方面，AI 模型可以预测最佳辅料组合，提高药物稳定性和生物利用度。AI 还能预测药物与辅料之间的相互作用，避免潜在的不相容性。提高药物溶解度与生物利用度 药物的溶解度和生物利用度是影响其疗效的关键因素，近 40% 新开发的化学实体存在水溶性差的问题。机器学习模型可以通过对分子性质和溶解度数据的学习，预测药物在水性介质中的溶解度，并协助设计提高溶解度的制剂策略，如固体分散体、纳米化等技术。同时，AI 还能综合考虑多种因素，预测药物在人体内的吸收速率和药代动力学特征。纳米载体与靶向递送系统设计 纳米医学的发展需要精准设计纳米载体，AI 在这方面发挥了重要作用。通过对实验数据的学习，AI 算法可以优化纳米颗粒的设计，提高药物靶向性，减少对其他组织的副作用。AI 还能预测最有效的配体组合，增强纳米载体与目标细胞的结合能力，提升纳米医学的治疗效果。AI 在制药行业的实际案例制药巨头的 AI 应用实践 众多制药公司已广泛应用 AI 技术。辉瑞在新冠疫苗生产中，利用 AI 优化生产流程，提高产量并缩短生产时间，同时运用机器学习算法预测产品温度，进行预防性维护，确保疫苗质量。强生通过数字孪生技术，模拟和优化生产过程，提高产品上市速度。诺华利用 AI 优化供应链物流，改善库存管理，降低运营成本。AI 助力药物研发突破 一些生物技术公司借助 AI 在药物研发上取得了显著成果。Insilico Medicine 利用内部 AI 算法，在 18 个月内就开发出了针对特发性肺纤维化的新型药物候选物。Exscientia 运用 AI 设计出了高活性、高选择性的蛋白激酶 C - θ 抑制剂 EXS4318，为治疗自身免疫性疾病带来了新希望。 AI 在制药行业面临的挑战与未来展望 尽管 AI 在制药行业取得了显著进展，但仍面临诸多挑战。数据质量和可用性是关键问题，高质量数据是训练有效 AI 模型的基础。AI 模型的可解释性也至关重要，复杂的模型常被视为 “黑箱”，难以解释其决策过程，这对监管审批和临床信任构成挑战。随着 AI 在制药领域的应用日益广泛，监管方面也需要建立相应的指导方针和标准，确保 AI 驱动的方法安全有效。 展望未来，AI 在制药行业将发挥更大的作用。随着基因组数据的不断丰富，AI 与基因组学的融合将进一步推动个性化医疗的发展。AI 驱动的预测分析将更精准地预测市场趋势、患者行为和潜在不良反应，提高药物安全性和有效性。监管机构也将逐步适应 AI 技术的发展，制定合理的政策，在保障安全有效的同时，促进创新。AI 在制药行业的发展将为全球医疗健康领域带来更多创新解决方案，提升药物研发效率，改善患者治疗效果，推动医疗行业的变革与发展。 识别微信二维码，添加生物制品圈小编，符合条件者即可加入 生物制品微信群！ 请注明：姓名+研究方向！ 版 权 声 明 本公众号所有转载文章系出于传递更多信息之目的，且明确注明来源和作者，不希望被转载的媒体或个人可与我们联系(cbplib@163.com)，我们将立即进行删除处理。所有文章仅代表作者观，不代表本站立。

CDK4, or cyclin-dependent kinase 4, is a crucial protein involved in cell cycle regulation in the human body. It plays a significant role in controlling the progression of cells from the G1 phase to the S phase, where DNA replication occurs. CDK4 forms a complex with cyclin D, which activates its kinase activity. This activation leads to the phosphorylation of key proteins involved in cell cycle progression, allowing cells to transition from the resting phase to the active phase of cell division. Dysregulation of CDK4 activity has been associated with various diseases, including cancer, making it an important target for pharmaceutical interventions. CDK4 Competitive LandscapeAccording to the data provided by Patsnap Synapse-Global Drug Intelligence Database: as of 10 Sep 2023, there are a total of 76 CDK4 drugs worldwide, from 104 organizations, covering 91 indications, and conducting 1053 clinical trials. The analysis of the target CDK4 reveals a competitive landscape with multiple companies actively involved in the development of drugs. Novartis AG, Pfizer Inc., and G1 Therapeutics, Inc. are leading in terms of R&D progress. The indications with the highest number of approved drugs include hormone receptor-positive HER2-negative breast cancer, breast cancer, and metastatic breast cancer. Small molecule drugs are progressing rapidly under the target CDK4, indicating intense competition. Biosimilars, such as biological products, are also present, suggesting competition around the innovative small molecule drugs. The countries/locations developing fastest include China, the United States, the European Union, Australia, and Canada. Overall, the target CDK4 presents a competitive landscape with a focus on developing drugs for various indications. Further analysis of the research and development institutions involved in biosimilar development and the progress in China will provide a comprehensive understanding of the current competitive landscape and future development opportunities for CDK4-targeted drugs. Key Drug: Palbociclib Palbociclib is a small molecule drug that targets CDK4 and CDK6. It has been approved for use in various therapeutic areas, including skin and musculoskeletal diseases, neoplasms, urogenital diseases, immune system diseases, digestive system disorders, endocrinology and metabolic disease, and hemic and lymphatic diseases. The drug has shown efficacy in treating metastatic breast cancer, hormone receptor positive HER2 negative breast cancer, estrogen receptor positive breast cancer, colorectal cancer, mantle-cell lymphoma, prostatic cancer, liver cancer, pancreatic cancer, renal cell carcinoma, and dermatitis. Palbociclib was developed by Pfizer Inc., a leading pharmaceutical company. It received its first approval in the United States in February 2015. The drug has also been approved in China. The regulatory process for Palbociclib involved priority review, accelerated approval, breakthrough therapy designation, and special review project. The approval of Palbociclib marks a significant advancement in the treatment of various cancers and other diseases. By targeting CDK4 and CDK6, the drug inhibits the progression of cancer cells and has shown promising results in clinical trials. Its approval for multiple indications demonstrates its potential to address unmet medical needs across different patient populations. The therapeutic areas in which Palbociclib is approved cover a wide range of diseases, indicating its versatility and potential for future applications. The drug's approval for metastatic breast cancer and hormone receptor positive HER2 negative breast cancer is particularly significant, as these are common types of breast cancer that often require targeted therapies. The originator organization, Pfizer Inc., has a strong track record in developing innovative pharmaceuticals. The approval of Palbociclib further solidifies Pfizer's position as a leader in the pharmaceutical industry. In conclusion, Palbociclib is a small molecule drug that targets CDK4 and CDK6. It has been approved for various therapeutic areas, including multiple types of cancer and dermatitis. Developed by Pfizer Inc., the drug has received approvals in the United States and China. Its approval marks a significant advancement in the treatment of cancer and other diseases, offering new hope for patients in need. Abemaciclib Abemaciclib is a small molecule drug that targets CDK4 and CDK6. It has been approved for various therapeutic areas including neoplasms, skin and musculoskeletal diseases, immune system diseases, digestive system disorders, hemic and lymphatic diseases, urogenital diseases, nervous system diseases, endocrinology and metabolic diseases, and respiratory diseases. The drug has shown efficacy in treating several types of cancers, such as HR positive/HER2 negative/node positive breast cancer, hormone receptor positive HER2 negative breast cancer, metastatic hormone-sensitive prostate cancer (mHSPC), ER-positive/HER2-negative breast cancer, prostatic cancer, meningioma, gastroesophageal junction adenocarcinoma, mesothelioma, malignant, adenocarcinoma of esophagus, cholangiocarcinoma, glioblastoma, endometrial carcinoma, pancreatic cancer, sarcoma, mantle-cell lymphoma, colonic cancer, retroperitoneal sarcoma, metastatic hormone refractory prostate cancer, renal cell carcinoma, colorectal cancer, melanoma, cutaneous malignant, microsatellite instability-high cancer, lymphoma, non-Hodgkin lymphoma, and PIK3CA H1047R mutant ER-positive, HER2-negative breast cancer. Abemaciclib was developed by Eli Lilly & Co. and received its first approval in the United States in September 2017. It has also been approved in China. The drug has undergone various regulatory processes, including priority review, fast track designation, breakthrough therapy designation, and special review project. In summary, Abemaciclib is a small molecule drug that targets CDK4 and CDK6. It has been approved for the treatment of multiple cancers and has shown promising results in various therapeutic areas. Its approval in both the United States and China highlights its global significance. The drug has undergone rigorous regulatory processes, indicating its potential as a breakthrough therapy. The content above comes from the network. if any infringement, please contact us to modify.

The KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) gene is a GDP/GTP binding protein. KRAS is in the activated state when bound to GTP, and in the deactivated state when bound to GDP. KRAS can be briefly activated by growth factors or tyrosine kinases such as EGFR. The activated KRAS can then activate downstream pathways such as the PI3K-AKT-mTOR pathway, which controls cell generation, and the RAS-RAF-MEK-ERK pathway, which controls cell proliferation. Mutated KRAS becomes continuously activated, even in the absence of kinase activation such as EGFR, which leads to continuous cell proliferation and ultimately oncogenesis. Research has found that KRAS G12C is a specific sub-mutation of KRAS, where the 12th codon's glycine is replaced by cysteine. It accounts for about 44% of all KRAS mutations. Among them, it is most common in non-small cell lung adenocarcinomas (14%), followed by colorectal adenocarcinomas (3-4%), and pancreatic cancers (2%). Globally, more than 100,000 people are diagnosed with the KRAS G12C mutation each year. KRAS G12C is a specific mutation of the KRAS gene that plays a crucial role in the development and progression of certain cancers. This mutation occurs in the KRAS protein, which is involved in regulating cell growth and division. In the human body, KRAS G12C mutation is commonly found in lung, colorectal, and pancreatic cancers. It leads to the activation of abnormal signaling pathways, promoting uncontrolled cell proliferation and tumor growth. Understanding the role of KRAS G12C is essential for developing targeted therapies that can specifically inhibit this mutation, offering potential treatment options for patients with KRAS G12C-mutated cancers. KRAS G12C Competitive LandscapeAccording to the data provided by Patsnap Synapse-Global Drug Intelligence Database: as of 11 Sep 2023, there are a total of 78 KRAS G12C drugs worldwide, from 79 organizations, covering 27 indications, and conducting 182 clinical trials. Several drugs under the target KRAS G12C have been approved for relevant indications. These indications include KRAS G12C mutant Non-small Cell Lung Cancer, Advanced Lung Non-Small Cell Carcinoma, metastatic non-small cell lung cancer, Colorectal Cancer, Endometrial Carcinoma, and Neoplasms. The drug types that are progressing most rapidly under the target KRAS G12C include small molecule drugs, PROTACs, oligonucleotides, TCR therapy, chemical drugs, biological products, small interfering RNA, and mRNA. Small molecule drugs have the highest number of drugs in approved, preclinical, and inactive stages. China has shown significant progress in the development of drugs targeting KRAS G12C. They have drugs in Phase 3, preclinical, and inactive stages. Other countries such as the United States, European Union, Japan, and the United Kingdom also have a considerable number of drugs in advanced stages of development. Overall, the target KRAS G12C presents a competitive landscape with multiple companies and drug types involved in its development. The future development of this target holds promise for the treatment of various types of cancers, particularly those associated with KRAS G12C mutations. Key drug:Sotorasib Sotorasib is a small molecule drug developed by Amgen, Inc. It falls under the category of biomedicine and is primarily used to target KRAS G12C, a specific mutation found in various types of cancers. The drug has shown potential therapeutic benefits in the treatment of neoplasms, digestive system disorders, and respiratory diseases. Sotorasib's active indications include advanced lung non-small cell carcinoma, KRAS G12C mutant non-small cell lung cancer, non-small cell lung cancer, KRAS p.G12C mutant colorectal cancer, colorectal cancer, and solid tumors. These indications highlight the drug's potential in treating a wide range of cancers, particularly those associated with the KRAS G12C mutation. Sotorasib received its first approval in the United States in May 2021, making it available for use in the American market. The drug's regulatory status includes accelerated approval, fast track designation, breakthrough therapy designation, and orphan drug designation. These regulatory designations highlight the potential significance and urgency of Sotorasib in addressing unmet medical needs and providing innovative treatment options for patients. In summary, Sotorasib is a small molecule drug developed by Amgen, Inc. that specifically targets the KRAS G12C mutation. It has shown promise in treating various types of cancers, including advanced lung non-small cell carcinoma and colorectal cancer. With its recent approval in the United States and ongoing phase 3 development in China, Sotorasib represents a significant advancement in the field of biomedicine and offers potential therapeutic benefits for patients with specific genetic mutations. Adagrasib Adagrasib is a small molecule drug that targets the KRAS G12C mutation. It has shown potential therapeutic benefits in various therapeutic areas, including neoplasms, digestive system disorders, endocrinology and metabolic disease, and respiratory diseases. The drug is specifically indicated for KRAS G12C mutant non-small cell lung cancer, metastatic non-small cell lung cancer, colorectal cancer, KRAS G12C mutant colorectal cancer, non-small cell lung cancer, solid tumors, pancreatic cancer, and KRAS G12C mutation solid tumors. The first approval of Adagrasib was granted in the United States, with a scheduled date of December 2022. The approval of Adagrasib is significant in the field of biomedicine, particularly in the treatment of cancers associated with the KRAS G12C mutation. This mutation is found in various types of cancer and has been challenging to target effectively. Adagrasib's approval offers new hope for patients with KRAS G12C mutant non-small cell lung cancer, colorectal cancer, and other solid tumors. As a small molecule drug, Adagrasib has the potential for oral administration, which may provide convenience for patients compared to other treatment options. The drug's approval in the United States and ongoing phase 3 trials in China indicate its potential for global availability and impact. In conclusion, Adagrasib is a small molecule drug developed by Array BioPharma, Inc. and Mirati Therapeutics, Inc. It targets the KRAS G12C mutation and has shown promise in various therapeutic areas, particularly in the treatment of cancers such as non-small cell lung cancer, colorectal cancer, and pancreatic cancer. The drug has received regulatory designations and is expected to receive its first approval in the United States in December 2022. Its approval offers new treatment options for patients with KRAS G12C mutant cancers and represents a significant development in the field of biomedicine. The content above comes from the network. if any infringement, please contact us to modify.